2. GPCR/G Protein Neuronal Signaling
  3. GPR119
  4. AZ13581837

AZ13581837 是一种具有口服活性的 GPR120 激动剂，对人源的 EC50 值为 5.2 nM，对小鼠的 EC50 为 4.3 nM。AZ13581837 可通过 Gαq、Gαs 和 β-arrestin 通路传递信号，抑制 cAMP 的生成，促进 GLP-1 分泌，诱导血糖降低并增加胰岛素分泌。AZ13581837 可用于 2 型糖尿病的相关研究。

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AZ13581837

AZ13581837 Chemical Structure

CAS No. : 2896777-27-6

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AZ13581837 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZ13581837 is a GPR120 agonist with oral effectiveness, human EC50 values of 5.2 nM, and mouse EC50 of 4.3 nM. AZ13581837 signals through Gαq, Gαs, and β-arrestin pathways, reduces cAMP production, stimulates GLP-1 secretion, induces glucose lowering, and increases insulin secretion. AZ13581837 can be used for the research of type 2 diabetes[1].

体外研究
(In Vitro)

AZ13581837 (1×10−9 to 1×10−4 M) 可强效激活 CHO-hGPR120 细胞中的人源 GPR120，诱导 GPR120 特异性 DMR 反应，其 EC50 为 5.2 nM[1]。
AZ13581837 (1×10−9 to 1×10−4 M) 可强效激活 CHO-mGPR120 细胞中的小鼠 GPR120，诱导 DMR 反应，其 EC50 为 4.3 nM[1]。
AZ13581837 (1×10−9 to 1×10−4 M) 可在 CHO-hGPR120 细胞中诱导依赖 Gαq 的钙动员反应，其 EC50 为 120 nM[1]。
AZ13581837 (1×10-9 to 1×10-4 M; 45 min) 可通过 Gαs 信号通路刺激 CHO-hGPR120 细胞中 cAMP 的生成，其 EC50 为 60 nM[1]。
AZ13581837 (1×10−9 to 1×10−4 M; 5 h) 可在 U2OS-hGPR120 细胞中强效诱导 β-arrestin 招募，其 EC50 为 5.2 nM[1]。
AZ13581837 (10 μM; 30 min) 可特异性抑制原代野生型小鼠胰岛细胞中 cAMP 的生成，而在 GPR120 敲除胰岛细胞中未观察到该作用[1]。
AZ13581837 (10 μM; 2 h) 可诱导 STC-1 肠内分泌细胞显著分泌 GPR120 依赖性的活性 GLP-1[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AZ13581837 相关抗体:

ELISA Assay[1]

Cell Line: STC-1 mouse enteroendocrine cells
Concentration: 10 μM
Incubation Time: 2 h
Result: Significantly increased active GLP-1 secretion from STC-1 cells compared to vehicle control, with secreted active GLP-1 levels.
体内研究
(In Vivo)

AZ13581837 (7-18 mg/kg；口服；葡萄糖负荷前 30 分钟单次给药) 可改善瘦雄性小鼠的口服葡萄糖耐量，其 CE50 为 0.02 μM，在 18 mg/kg 时可观察到显著效应[1]。
AZ13581837 (35 mg/kg；口服；葡萄糖冲击前 30 分钟单次给药) 可通过 GLP-1 依赖性机制增强瘦型雌性小鼠的葡萄糖刺激胰岛素分泌并改善葡萄糖清除[1]。
AZ13581837 (35 mg/kg；口服；葡萄糖冲击前 30 分钟单次给药) 具有依赖于功能性 GPR120 的降血糖和促胰岛素分泌作用，因为在 GPR120 基因敲除小鼠中未观察到上述作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (8-week-old male, 27-32 g)[1]
Dosage: 7 mg/kg; 18 mg/kg
Administration: p.o.; single dose 30 minutes prior to glucose load
Result: Caused a concentration-dependent reduction in glucose excursions compared to vehicle-treated mice.
Resulted in significantly improved glucose tolerance at 18 mg/kg dose.
Achieved an unbound effective concentration (Ce50) of 0.02 μM, corresponding to exposure levels 1-3 times the in vitro EC50 for mouse GPR120 in the DMR assay.
Animal Model: C57BL/6JOlaHSd (8-week-old female, 20-25 g)[1]
Dosage: 35 mg/kg
Administration: p.o.; single dose 30 minutes prior to glucose bolus
Result: Caused a slight but significant reduction in basal blood glucose (7.1 mM.
Significantly elevated insulin levels up to 10 minutes post glucose bolus.
Increased the acute insulin response (AIR) to ~2.4 ng/mL.
Significantly reduced plasma glucose at 20 minutes post glucose bolus.
Increased glucose elimination to ~3.8%/min.
Induced a significant increase in total GLP-1 levels compared to vehicle-treated mice.
Animal Model: C57BL/6 wild-type (female, 22.5-23.0 g); C57BL/6 GPR120 null (female, 22.5 ± 0.7 g)[1]
Dosage: 35 mg/kg
Administration: p.o.; single dose 30 minutes prior to glucose bolus
Result: Significantly increased the acute insulin response compared to vehicle controls and increased glucose elimination in wild-type mice.
分子量

362.40

Formula

C20H14N2O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AZ13581837 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZ135818372896777-27-6AZ 13581837AZ-13581837GPR119G Protein-Coupled Receptor 119GαqCHO-mGPR120 cellstype 2 diabetesCHO-hGPR120 cellsGPR120GLP-1GαsSTC-1 enteroendocrine cellscAMPβ-arrestinInhibitorinhibitorinhibit

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